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PTC299

Chemical Structure : PTC299

CAS No.: 1256565-36-2

PTC299 (Emvododstat, PTC-299, PTC 299)

货号: PC-35755Not For Human Use, Lab Use Only.

Emvododstat (PTC299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Emvododstat (PTC299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.
PTC299 inhibited DHODH activity more potently than teriflunomide and with potency similar to that of brequinar.
PTC299 demonstrates broad and potent activity against hematological cancer cells in preclinical models, inhibits AML patient-derived cells with IC50 of 2-60 nM.
PTC299 demonstrates advantages over previously reported DHODH inhibitors, including greater potency, good oral bioavailability and lack of off-target kinase inhibition and myelosuppression.

物理化学性质&存储条件

分子量 467.346
分子式 C25H20Cl2N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO (46.7 mg/mL, ultrasonic needed)

Chemical Name/SMILES

4-chlorophenyl (S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole-2-carboxylate

参考文献

1. Cao L, et al. Mol Cancer Ther. 2018 Oct 23. pii: molcanther.0863.2018.

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